KR20160021243A - 알킬 플루오로알킬 술포네이트를 사용한 알킬화 - Google Patents

알킬 플루오로알킬 술포네이트를 사용한 알킬화 Download PDF

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Publication number
KR20160021243A
KR20160021243A KR1020167001145A KR20167001145A KR20160021243A KR 20160021243 A KR20160021243 A KR 20160021243A KR 1020167001145 A KR1020167001145 A KR 1020167001145A KR 20167001145 A KR20167001145 A KR 20167001145A KR 20160021243 A KR20160021243 A KR 20160021243A
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KR
South Korea
Prior art keywords
alkyl
base
tert
formula
protecting group
Prior art date
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KR1020167001145A
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English (en)
Korean (ko)
Inventor
무라트 아체모글루
젬마 바이치
Original Assignee
노파르티스 아게
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Application filed by 노파르티스 아게 filed Critical 노파르티스 아게
Publication of KR20160021243A publication Critical patent/KR20160021243A/ko

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/18Bridged systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/436Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having oxygen as a ring hetero atom, e.g. rapamycin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C303/00Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides
    • C07C303/26Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides of esters of sulfonic acids
    • C07C303/28Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides of esters of sulfonic acids by reaction of hydroxy compounds with sulfonic acids or derivatives thereof
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/63Esters of sulfonic acids
    • C07C309/64Esters of sulfonic acids having sulfur atoms of esterified sulfo groups bound to acyclic carbon atoms
    • C07C309/65Esters of sulfonic acids having sulfur atoms of esterified sulfo groups bound to acyclic carbon atoms of a saturated carbon skeleton
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02Silicon compounds
    • C07F7/08Compounds having one or more C—Si linkages
    • C07F7/18Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
    • C07F7/1804Compounds having Si-O-C linkages
    • C07F7/1856

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Immunology (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Transplantation (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
KR1020167001145A 2013-06-20 2014-06-18 알킬 플루오로알킬 술포네이트를 사용한 알킬화 KR20160021243A (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201361837224P 2013-06-20 2013-06-20
US61/837,224 2013-06-20
PCT/IB2014/062375 WO2014203185A1 (en) 2013-06-20 2014-06-18 Alkylation with an alkyl fluoroalkyl sulfonate

Publications (1)

Publication Number Publication Date
KR20160021243A true KR20160021243A (ko) 2016-02-24

Family

ID=51014598

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1020167001145A KR20160021243A (ko) 2013-06-20 2014-06-18 알킬 플루오로알킬 술포네이트를 사용한 알킬화

Country Status (13)

Country Link
US (1) US20160130280A1 (da)
EP (1) EP3010926B1 (da)
JP (1) JP6574173B2 (da)
KR (1) KR20160021243A (da)
CN (2) CN109651396B (da)
AU (1) AU2014282831B2 (da)
BR (1) BR112015029521A2 (da)
CA (1) CA2911104A1 (da)
HK (1) HK1219727A1 (da)
IL (1) IL242413B (da)
MX (1) MX2015017536A (da)
RU (1) RU2691728C2 (da)
WO (1) WO2014203185A1 (da)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN104592254B (zh) * 2015-02-08 2016-07-13 福建省微生物研究所 依维莫司的合成方法
CN104876944B (zh) * 2015-05-13 2017-11-10 普济生物科技(台州)有限公司 一种依维莫司的制备方法
EP3109250A1 (en) * 2015-06-23 2016-12-28 Synbias Pharma AG Method for the synthesis of rapamycin derivatives
CN108047265A (zh) * 2017-11-24 2018-05-18 成都海创药业有限公司 一种依维莫司中间体的制备纯化方法
RU2716714C1 (ru) * 2019-08-26 2020-03-16 Закрытое Акционерное Общество "Биокад" Новый способ получения эверолимуса
CZ308817B6 (cs) * 2019-09-12 2021-06-09 Ratiochem, s.r.o. Způsob výroby Everolimu
JP2023028473A (ja) * 2021-08-19 2023-03-03 日本マイクロバイオファーマ株式会社 エベロリムスの製造方法

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9221220D0 (en) * 1992-10-09 1992-11-25 Sandoz Ag Organic componds
WO1996041807A1 (en) * 1995-06-09 1996-12-27 Novartis Ag Rapamycin derivatives
CN1235608A (zh) * 1996-09-09 1999-11-17 美国家用产品公司 烷基化的雷帕霉素衍生物
JP4716280B2 (ja) * 2004-03-01 2011-07-06 テルモ株式会社 O−アルキル化ラパマイシン誘導体の製造法
ATE418559T1 (de) 2004-03-01 2009-01-15 Terumo Corp Verfahren zur herstellung von o-alkylierten rapamycinderivaten
ES2296516B1 (es) 2006-04-27 2009-04-01 Laboratorios Almirall S.A. Derivados de 4-(2-amino-1-hidroxietil)fenol como agonistas del receptor beta2 adrenergico.
TW200948361A (en) * 2008-05-26 2009-12-01 Chunghwa Chemical Synthesis & Biotech Co Ltd Method for synthesizing Biolimus A9 and the like and method for improving stability of the same
CN102127092B (zh) * 2010-01-18 2013-04-17 东南大学 依维莫斯的制备
CA2818225C (en) * 2010-11-19 2016-10-25 Biocon Limited Processes for preparation of everolimus and intermediates thereof
WO2012103959A1 (en) * 2011-02-04 2012-08-09 Synthon Bv Process for making everolimus

Also Published As

Publication number Publication date
CN105324386A (zh) 2016-02-10
JP2016523246A (ja) 2016-08-08
RU2015156316A (ru) 2017-07-25
HK1219727A1 (zh) 2017-04-13
EP3010926B1 (en) 2019-11-20
AU2014282831B2 (en) 2016-12-01
BR112015029521A2 (pt) 2017-07-25
AU2014282831A1 (en) 2015-11-12
JP6574173B2 (ja) 2019-09-11
CN109651396B (zh) 2021-09-14
RU2691728C2 (ru) 2019-06-18
MX2015017536A (es) 2016-04-26
CA2911104A1 (en) 2014-12-24
CN105324386B (zh) 2019-02-19
CN109651396A (zh) 2019-04-19
EP3010926A1 (en) 2016-04-27
US20160130280A1 (en) 2016-05-12
IL242413B (en) 2018-04-30
WO2014203185A1 (en) 2014-12-24

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